Konorev Pharm Lect Drug Targets Flashcards
what do protein kinases do?
phosphorylate proteins
What 2 things are present at a MAJORITY of signal pathways?
Protein kinases and transcription factors
what are transcription factors?
proteins that bind to specific DNA sequences and control the transcription of genetic information from DNA to RNA
where does a transcription factor bind?
to an enhancer or promoter of DNA adjacent to coding sequence of regulated gene
what is the name of the specific DNA sequence that the transcription factor binds to?
response element
T/F when a trimeric G-protein is activated the affinity of its Alpha subunit for GTP is decreased?
F
what is the other name for a GPCR?
7 transmembrane or 7 pass domain
what family of G proteins activate all isoforms of AC and Scr tyrosine kinase?
Gs
what G protein family activates phospholipase CB(beta)?
Gq
what family of GPCR inhibitis AC 13, 5, 6 but activates tyrosine kinase Src?
Gi
What type of molecules do transcription factors interact with to fulfill their main function?
DNA
Diacylglycerol is lipophilic intermediate that activates…?
Protein Kinase C
which endogenous ligand activates receptor tyrosine kinase?
insulin
SH2 domain of RTK binds to?
phosphorylated tyrosines
SH3 domain binds to?
the proline-rich sequences
which proteins contain a variety of protein-binding domains that link protein partners together and facilitate the creation of larger signaling complexes?
adaptor proteins
what kinds of ligands are lipophilic, examples?
steroid hormones, thyroid hormones, Vit A, Vit C, and lipid mediates, free fatty acids and their products
permeability to what ion is increased as a result of activation of a nicotinic receptor?
mostly Na+
GABA is an inhibitory neurotransmitter as binding of GABA to its cognate receptor ion channel will cause
influx of Cl-
voltage gated channels are activated by what?
depolarization of the membrane
what composes fast Na+ channels? where are these present?
alpha and beta subunit, all excitable tissue
what are some examples of drugs that inhibit voltage-gated Na+ channels?
local anesthetics (lidocaine), antiarrhythmic drugs (quinidine), drugs used to tx epilepsy (phenytoine)
A 55yo man with CAD is tx with an antihyperlipidemic drug. Drugs A and B have the same mechanism of lowering the blood lipid levels. Drug A in a dose of 1mg produces the same magnitude of lipid lowering as 20mg of Drug B. what does this suggest?
drug B is more potent
A physician considersd two medications Drug A and B to tx her pt. Drug A is a partial agonist
finish this later
